- 1-[(1-methyl-1 H-imidazol-2-yl)methyl]-4-phenylpiperidines as mGluR2 positive allosteric modulators for the treatment of psychosis
-
A novel series of mGluR2 positive allosteric modulators (PAMs), 1-[(1-methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines, is herein disclosed. Structure-activity relationship studies led to potent, selective mGluR2 PAMs with excellent pharmacokinetic profiles. A representative lead compound (+)-17e demonstrated dose-dependent inhibition of methamphetamine-induced hyperactivity and mescaline-induced scratching in mice, providing support for potential efficacy in treating psychosis.
- Zhang, Lei,Brodney, Michael A.,Candler, John,Doran, Angela C.,Duplantier, Allen J.,Efremov, Ivan V.,Evrard, Edel,Kraus, Kenneth,Ganong, Alan H.,Haas, Jessica A.,Hanks, Ashley N.,Jenza, Keith,Lazzaro, John T.,Maklad, Noha,McCarthy, Sheryl A.,Qian, Weimin,Rogers, Bruce N.,Rottas, Melinda D.,Schmidt, Christopher J.,Siuciak, Judith A.,Tingley III, F. David,Zhang, Andy Q.
-
experimental part
p. 1724 - 1739
(2011/05/07)
-
- BENZIMIDAZOLYL COMPOUNDS AS POTENTIATORS OF MGLUR2 SUBTYPE OF GLUTAMATE RECEPTOR
-
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
- -
-
Page/Page column 70-71
(2010/11/30)
-
- AZABENZIMIDAZOLYL COMPOUNDS
-
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
- -
-
Page/Page column 66
(2008/06/13)
-
